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Compound Detail

CHEMBL254349

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CC(C)CN(C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)O[C@@H]1C[C@@H]2CCO[C@@H]2C1)S(=O)(=O)c1ccc(CO)cc1

Basic Information

ChEMBL ID CHEMBL254349
Phase Preclinical
Structure Type MOL
InChI Key VYBDPVQMILRSMK-GRXYLYAXSA-N
2
Targets
6
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

560.7
MW (Da)
3.09
ALogP
7
HBA
3
HBD
125.4
PSA (Ų)
0.36
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H40N2O7S
MW 560.71
Aromatic Rings 2
Heavy Atoms 39
NP-Likeness 0.19

Activity Summary

IC50 3 meas. best 8.85
Ki 3 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Human immunodeficiency virus 1
CHEMBL378
IC50 8.85 8.85 1.4 1
Protease
CHEMBL2366517
IC50 8.74 8.74 1.8 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Human immunodeficiency virus 1 IC50 = 1.4 nM 8.85 Antiviral activity against HIV1 LAI in MT2 cells 17635930
Protease IC50 = 1.8 nM 8.74 Inhibition of HIV1 protease 17900913
Protease IC50 = 1.8 nM 8.74 Inhibition of HIV1 protease 19323561

Literature References

PubMed DOI Target Context # Activities
17900913 10.1016/j.bmc.2007.09.010 Protease 2
17635930 10.1074/jbc.m703938200 Protease 2
19323561 10.1021/jm900064c Protease 2
17635930 10.1074/jbc.m703938200 Human immunodeficiency virus 1 1

Data from ChEMBL 36 via Core Engine